Proteolysis targeting chimeric molecule, preparation method, and application

US11504385B2 · kind B2 · utility

Assignee

• CHINA PHARMACEUTICAL UNIVERSITY · CN

Inventors

• Qidong You · 安丰镇, CN
• Zhengyu JIANG · Nanjing, CN
• Yan Wang · Jingwei, CN
• Yuhui Jin · Corning, US
• Mengchen Lu · Nanjing, CN
• Xiaoli Xu · Shanghai, CN
• Xiaoke GUO · 安丰镇, CN

Key dates

• Filing date: Sep 4, 2019
• Grant date: Nov 22, 2022
• Expiry date: Sep 4, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.